CC-90011
- Product NameCC-90011
- CAS2097523-60-7
- CBNumberCB55544449
- MFC30H29F2N5O5S
- MW609.65
- EINECS-0
- MDL NumberMFCD32644589
- MOL File2097523-60-7.mol
Chemical Properties
| solubility | DMSO:62.5(Max Conc. mg/mL);102.52(Max Conc. mM) |
| form | Solid |
| color | Off-white to light yellow |
CC-90011 Chemical Properties,Usage,Production
Uses
CC-90011 benzenesulfonate is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. CC-90011 benzenesulfonate is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. CC-90011 benzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity[1].in vivo
CC-90011 (5 mg/kg; oral administration; daily; for 30 days) treatment inhibits tumor growth in patient-derived xenograft SCLC models[1].
CC-90011 (once a day; for 4 days) treatment results in robust downregulation of GRP mRNA levels at 2.5 mg/kg and maximum suppression of GRP at 5 mg/kg in a SCLC human tumor xenograft (H1417) mice[1].
After i.v. administration, CC-90011 (Compound 11; 5 mg/kg) has systemic clearance of 32.4 mL/min/kg, elimination half-life of 2 h, and a high volume of distribution of 7.5 L/kg. CC-90011 (Compound 11; 5 mg/kg) is readily absorbed after oral administration with an AUC0-24h of 1.8 μM·h, C/sub>max of 0.36 μM, and oral bioavailability of 32%[1].
| Animal Model: | BALB/c nude mice bearing small cell lung carcinoma (SCLC)[1] |
| Dosage: | 5 mg/kg |
| Administration: | Oral administration; daily; for 30 days |
| Result: | Showed a tumor growth inhibition (TGI) of 78% at 5 mg/kg with no body weight loss. |
IC 50
KDM1/LSD1References
[1] Toufike Kanouni, et al. Discovery of CC-90011: A Potent and Selective Reversible Inhibitor of Lysine Specific Demethylase 1 (LSD1). J Med Chem. 2020 Dec 10;63(23):14522-14529. DOI:10.1021/acs.jmedchem.0c00978CC-90011 Suppliers
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